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CB1 RECEPTOR MODULATORS
专利权人:
发明人:
申请号:
EP07848570.3
公开号:
EP2121617B1
申请日:
2007.12.17
申请国别(地区):
EP
年份:
2014
代理人:
摘要:
Compounds of formula (I) suppress the normal signalling activity CB1 receptors, and are thus useful in the treatment of diseases or conditions which are mediated by CB1 receptor signalling activity, such as treatment of obesity and overweight, prevention of weigh gain, treatment of diseases and conditions directly or indirectly associated with obesity and overweight: wherein A1 is hydrogen, -COOH, or tetrazolyl, and A2 is hydrogen, -COOH, or tetrazolyl, provided that one of A1 and A2 is either -COOH or tetrazolyl p is O or 1 and A3 is phenyl or cycloalkyl, either of which is optionally substituted with R4 and/or R5 q is O or 1 R3 is hydrogen, C1-C4 alkyl, cycloalkyi, -CF3, or -OR9 R4 and R5 independently -R9, -CN, -F, -Cl, -Br, -OR9, - NR7R8, -NR7COR6, -NR7SO2R6, -COR6, -SR9, -SOR9, or -SO2R6 R6 is C1-C4 alkyl, cycloalkyl, -CF3 or -NR7R8 R7 and R8 are independently hydrogen, C1-C4 alkyl, -CF3, or cycloaikyL R9 is hydrogen, C1-C4 alkyl, cycloalkyl, fully or partially fluorinated C1-C4 alkyl R1 is (i) a bond, or (ii) -(CH2)aB1(CH2)b- wherein a and b are independently O, 1, 2 or 3 provided that a+b is 1, 2 or 3 or (iii) -C(R10)(R11)-*, -C(R10)(R11)-O-*. -C(R10)(R11)CH2-*, -C(R10)(R11)CH2-O-*, - CH2C(R10)(R11)-*, -CH2C(R10)(R11)-O-*, -CH2-O-C(R10)(R11)-* or -C(R10)(R11)-O-CH2-*, wherein the bond indicated by an asterisk is attached to the pyrazole ring R2 is a divalent radical of formula -Q1A4-[Q2]w- wherein Q1, A4, Q2 and w are as defined in the specification and R10 is hydrogen and R11 is (C1-C3)alkyl or -OH or R10 and R11 are both (C1-C3)alkyl or R10 and R11 taken together with the carbon atom to which they are attached form a (C3- C5)cycloalkyl ring.Linvention concerne des composés de formule (I) supprimant lactivité de signalisation normale des récepteurs CB1 et qui sont utiles dans le traitement de maladies ou de troubles induits par lactivité de signalisation du récepteur CB1, notamment dans le traitement de lobésité et du surpoids, dans la prévention de prise de
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